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21.
Brillouin scattering (BS), photon correlation spectroscopy (PCS), and ultrasonic (US) measurements were conducted to study the curing process of diglycidyl ether of bisphenol A with butane-1,4-diol at a curing temperature of 100°C. The experimental techniques probe the primary glass-rubber transition during the curing reaction. The primary relaxation time τ obtained from the BS and US velocity and absorption increases with curing time and hence the BS experiment measures τ at earlier stages of cure than the US experiment. The relaxation times at a different extent of reaction and for different measuring temperatures are consistent with BS, US, PCS, and DSC measurements and conform to a single reduced Vogel–Fulcher–Hesse–Tamann equation. Furthermore, the US experiments show evidence of secondary relaxations in the epoxy system. 相似文献
22.
Homoionic Na+, Ca2+, Sr2+, Li+, Cu2+ and Zn2+ samples of the <2 μm fraction of a cis-vacant montmorillonite from Linden (Bavaria) were steam treated at 200°C (≈1.5 MPa), 240°C (≈3.3 MPa) and 300°C (≈8.0 MPa) after dehydroxylation at temperatures up to 630°C. Cation exchange capacity (CEC) measurements, determination of exchangeable cations and X-ray diffraction (XRD), supplemented by thermoanalytical investigations of the evolved water in a thermobalance linked to a mass spectrometer, infrared (IR) and electron spin resonance (ESR) spectroscopy were employed to obtain information about the state of expandability and structural changes of swellable montmorillonite and the sites of interlayer and octahedral cations after heating and rehydroxylation.The XRD pattern of the initial samples showed a well-defined (001) reflection according to the interlayer cation and its hydration state under laboratory atmosphere. After dehydroxylation the pattern exhibited (001) reflections between 9.6 and 9.8 Å, corresponding to a collapsed structure for all samples. The Na+-, Ca2+- and Sr2+-rich montmorillonites regained partial expandability after rehydroxylation at 200°C and full expandability after rehydroxylation at 300°C if the dehydroxylation temperature was less than 630°C. Rehydroxylation at 300°C of the Cu2+- and Zn2+-rich montmorillonites did not cause reexpansion, whereas the Li+-rich samples recovered a partial swellability after rehydroxylation at 240°C and nearly the full swellability after rehydroxylation at 300°C.The Li+-, Cu2+- and Zn2+-rich samples underwent a strong CEC reduction due to migration of the interlayer cations into the 2:1 layer before dehydroxylation started. After rehydroxylation under water steam Cu2+- and Zn2+-rich samples released 16–30 meq/100 g of Mg2+ from the structure, increasing with the steam temperature. Mg2+ release was not observed for the Li+-rich montmorillonite. 相似文献
23.
Neil Gerard Quigley Dr. Stefano Tomassi Dr. Francesco Saverio di Leva Dr. Salvatore Di Maro Dr. Frauke Richter Dr. Katja Steiger Prof. Dr. Susanne Kossatz Prof. Dr. Luciana Marinelli Dr. Johannes Notni 《Chembiochem : a European journal of chemical biology》2020,21(19):2836-2843
αvβ6 Integrin is an epithelial transmembrane protein that recognizes latency-associated peptide (LAP) and primarily activates transforming growth factor beta (TGF-β). It is overexpressed in carcinomas (most notably, pancreatic) and other conditions associated with αvβ6 integrin-dependent TGF-β dysregulation, such as fibrosis. We have designed a trimeric Ga-68-labeled TRAP conjugate of the αvβ6-specific cyclic pentapeptide SDM17 (cyclo[RGD-Chg-E]-CONH2) to enhance αvβ6 integrin affinity as well as target-specific in-vivo uptake. Ga-68-TRAP(SDM17)3 showed a 28-fold higher αvβ6 affinity than the corresponding monomer Ga-68-NOTA-SDM17 (IC50 of 0.26 vs. 7.4 nM, respectively), a 13-fold higher IC50-based selectivity over the related integrin αvβ8 (factors of 662 vs. 49), and a threefold higher tumor uptake (2.1 vs. 0.66 %ID/g) in biodistribution experiments with H2009 tumor-bearing SCID mice. The remarkably high tumor/organ ratios (tumor-to-blood 11.2; -to-liver 8.7; -to-pancreas 29.7) enabled high-contrast tumor delineation in PET images. We conclude that Ga-68-TRAP(SDM17)3 holds promise for improved clinical PET diagnostics of carcinomas and fibrosis. 相似文献
24.
Daniel Stubba Dr. Dennis Bensinger Janika Steinbacher Lilia Proskurjakov Álvaro Salcedo Gómez Dr. Uwe Schmidt Prof. Dr. Stefan Roth Prof. Dr. Katja Schmitz Prof. Dr. Boris Schmidt 《ChemMedChem》2019,14(23):2005-2022
The ubiquitin-proteasome system (UPS) is an established therapeutic target for approved drugs to treat selected hematologic malignancies. While drug discovery targeting the UPS focuses on irreversibly binding epoxyketones and slowly-reversibly binding boronates, optimization of novel covalent-reversibly binding warheads remains largely unattended. We previously reported α-ketoamides to be a promising reversible lead motif, yet the cytotoxic activity required further optimization. This work focuses on the lead optimization of phenoxy-substituted α-ketoamides combining the structure-activity relationships from the primed and the non-primed site of the proteasome β5 subunit. Our optimization strategy is accompanied by molecular modeling, suggesting occupation of P1′ by a 3-phenoxy group to increase β5 inhibition and cytotoxic activity in leukemia cell lines. Key compounds were further profiled for time-dependent inhibition of cellular substrate conversion. Furthermore, the α-ketoamide lead structure 27 does not affect escape response behavior in Danio rerio embryos, in contrast to bortezomib, which suggests increased target specificity. 相似文献
25.
Katja König Saša Novak Aldo R. Boccaccini Spomenka Kobe 《Journal of Materials Processing Technology》2010,210(1):96-103
The electrophoretic deposition (EPD) method was investigated for the preparation of compacts from nanosized alumina powders. Ethanol suspensions of commercially available nanosized transition alumina and α-alumina powders were used. In addition, submicron powders were also considered for comparison. Besides the influence of operational pH change, the influence of the addition of three different surfactants – two branched polyethylene imines with molecular masses 1800 and 10,000, and citric acid—on the zeta-potential of the particles in ethanol and afterwards on the EPD was investigated.The packing density of the green parts prepared by the EPD of nanosized α-alumina powders at 30 V/cm was low (the green density was 27 vol. % of the theoretical density—TD), and a bimodal pore size distribution was observed. In contrast, the packing density in deposits made with the transition alumina nanopowder was much higher (the green density was 42 vol. % of the TD) and a monomodal distribution of pores was observed. In general, for all the deposits made from nanosized alumina powders, the particle-packing density was found to be lower than for those made from the submicron alumina powders (a green density equal to 59 vol. % of the TD). 相似文献
26.
Thomas van Groen Dr. Inga Kadish Dr. Katja Wiesehan Dr. Susanne A. Funke Dr. Dieter Willbold Prof. Dr. 《ChemMedChem》2009,4(2):276-282
Plaque visualisation : We identified three different D ‐enantiomeric peptides that bind to Alzheimer's amyloid β (Aβ1‐42). As there is currently no definitive pre‐mortem diagnosis for Alzheimer's disease, we investigated the peptides' suitability as molecular probes for in vivo imaging in transgenic mouse models.
27.
Nasdala L Ruschel K Rhede D Wirth R Kerschhofer-Wallner L Kennedy AK Kinny PD Finger F Groschopf N 《Chimia》2010,64(10):705-711
The internal textures of crystals of moderately radiation-damaged monazite-(Ce) from Moss, Norway, indicate heavy, secondary chemical alteration. In fact, the cm-sized specimens are no longer mono-mineral monazite but rather a composite consisting of monazite-(Ce) and apatite pervaded by several generations of fractures filled with sulphides and a phase rich in Th, Y, and Si. This composite is virtually a 'pseudomorph' after primary euhedral monazite crystals whose faces are still well preserved. The chemical alteration has resulted in major reworking and decomposition of the primary crystals, with potentially uncontrolled elemental changes, including extensive release of Th from the primary monazite and local redeposition of radionuclides in fracture fillings. This seems to question the general alteration-resistance of orthophosphate phases in a low-temperature, 'wet' environment, and hence their suitability as potential host ceramics for the long-term immobilisation of radioactive waste. 相似文献
28.
Max Braune Nico Scherf Claudia Heine Katja Sygnecka Thanigaimalai Pillaiyar Chiara Parravicini Bernd Heimrich Maria P. Abbracchio Christa E. Müller Heike Franke 《International journal of molecular sciences》2021,22(21)
Characterization of new pharmacological targets is a promising approach in research of neurorepair mechanisms. The G protein-coupled receptor 17 (GPR17) has recently been proposed as an interesting pharmacological target, e.g., in neuroregenerative processes. Using the well-established ex vivo model of organotypic slice co-cultures of the mesocortical dopaminergic system (prefrontal cortex (PFC) and substantia nigra/ventral tegmental area (SN/VTA) complex), the influence of GPR17 ligands on neurite outgrowth from SN/VTA to the PFC was investigated. The growth-promoting effects of Montelukast (MTK; GPR17- and cysteinyl-leukotriene receptor antagonist), the glial cell line-derived neurotrophic factor (GDNF) and of two potent, selective GPR17 agonists (PSB-16484 and PSB-16282) were characterized. Treatment with MTK resulted in a significant increase in mean neurite density, comparable with the effects of GDNF. The combination of MTK and GPR17 agonist PSB-16484 significantly inhibited neuronal growth. qPCR studies revealed an MTK-induced elevated mRNA-expression of genes relevant for neuronal growth. Immunofluorescence labelling showed a marked expression of GPR17 on NG2-positive glia. Western blot and RT-qPCR analysis of untreated cultures suggest a time-dependent, injury-induced stimulation of GPR17. In conclusion, MTK was identified as a stimulator of neurite fibre outgrowth, mediating its effects through GPR17, highlighting GPR17 as an interesting therapeutic target in neuronal regeneration. 相似文献
29.
Katja F. Hellendahl Felix Kaspar Dr. Xinrui Zhou Zhaoyi Yang Prof. Dr. Zhen Huang Prof. Dr. Peter Neubauer Dr. Anke Kurreck 《Chembiochem : a European journal of chemical biology》2021,22(11):2002-2009
Selenium-modified nucleosides are powerful tools to study the structure and function of nucleic acids and their protein interactions. The widespread application of 2-selenopyrimidine nucleosides is currently limited by low yields in established synthetic routes. Herein, we describe the optimization of the synthesis of 2-Se-uridine and 2-Se-thymidine derivatives by thermostable nucleoside phosphorylases in transglycosylation reactions using natural uridine or thymidine as sugar donors. Reactions were performed at 60 or 80 °C and at pH 9 under hypoxic conditions to improve the solubility and stability of the 2-Se-nucleobases in aqueous media. To optimize the conversion, the reaction equilibria in analytical transglycosylation reactions were studied. The equilibrium constants of phosphorolysis of the 2-Se-pyrimidines were between 5 and 10, and therefore differ by an order of magnitude from the equilibrium constants of any other known case. Hence, the thermodynamic properties of the target nucleosides are inherently unfavorable, and this complicates their synthesis significantly. A tenfold excess of sugar donor was needed to achieve 40−48 % conversion to the target nucleoside. Scale-up of the optimized conditions provided four Se-containing nucleosides in 6–40 % isolated yield, which compares favorably to established chemical routes. 相似文献
30.
For the analysis of the 16 PAH (EFSA-PAH), which are classified as priority for different food groups by the Scientific Committee
on Food (SCF) and the Joint FAO/WHO Experts Committee on Food Additives (JECFA) in tea, a sensitive analytical Fast-GC/HRMS
method was used. The sample preparation included accelerated solvent extraction (ASE) and the highly automated clean up steps,
gel permeation chromatography and solid phase extraction. The analytical parameters, limit of detection (0.01–0.02 μg/kg)
and limit of quantification (0.03–0.06 μg/kg), were determined. The repeatability (RSD, n = 3) of different PAH in fruit tea ranged from 0.1 to 11%. It was observed that the total contents of the 16 PAH in tea samples
ranged from 14 to 2,662 μg/kg. The analysed tea samples showed an increasing presence of PAH in the following order: herbal
and fruit tea (n = 7) < black tea (n = 11) < green tea (n = 11) < white tea (n = 3) < mate-tea (n = 8). The correlation coefficient (R) between BaP and the sum of the 16 EFSA-PAH was established considering the contamination
amount in all the 40 tea samples analysed. 相似文献